Chemistry: molecular biology and microbiology – Micro-organism – tissue cell culture or enzyme using process... – Recombinant dna technique included in method of making a...
Reexamination Certificate
2002-09-20
2008-08-12
Nickol, Gary B. (Department: 1646)
Chemistry: molecular biology and microbiology
Micro-organism, tissue cell culture or enzyme using process...
Recombinant dna technique included in method of making a...
C435S320100, C435S325000, C435S252300, C435S173300, C435S068100, C530S333000, C530S350000, C702S019000, C702S020000, C702S022000, C536S023100, C536S024310
Reexamination Certificate
active
07410777
ABSTRACT:
Disclosed herein are constitutively activated, non-endogenous versions of endogenous human G protein-coupled receptors comprising (a) the following amino acid sequence region (C-terminus to N-terminus orientation) and/or (b) the following nucleic acid sequence region (3′ to 5′ orientation) transversing the transmembrane-6 (TM6) and intracellular loop-3 (IC3) regions of the GPCR:(a) P1AA15Xand/or(b) pcodon(AA-codon)15Xcodon,respectively. In a most preferred embodiment, P1and Pcodonare endogenous proline and an endogenous nucleic acid encoding region encoding proline, respectively, located within TM6 of the non-endogenous GPCR; AA15and (AA-codon)15are 15 endogenous amino acid residues and 15 codons encoding endogenous amino acid residues, respectively; and X and Xcodonare non-endogenous lysine and a non-endogenous nucleic acid encoding region encoding lysine, respectively, located within IC3 of the non-endogenous GPCR. Because it is most preferred that the non-endogenous human GPCRs which incorporate these mutations are incorporated into mammalian cells and utilized for the screening of candidate compounds, the non-endogenous human GPCR incorporating the mutation need not be purified and isolated per se (i.e., these are incorporated within the cellular membrane of a mammalian cell), although such purified and isolated non-endogenous human GPCRs are well within the purview of this disclosure.
REFERENCES:
patent: 5514578 (1996-05-01), Hogness et al.
patent: 5532157 (1996-07-01), Fink
patent: 5573944 (1996-11-01), Kirschner et al.
patent: 5639616 (1997-06-01), Liao et al.
patent: 5750353 (1998-05-01), Kopin et al.
patent: 5861309 (1999-01-01), Bard et al.
patent: 5891720 (1999-04-01), Moore et al.
patent: 5955308 (1999-09-01), Bergsma et al.
patent: 6555339 (2003-04-01), Liaw et al.
patent: 2135253 (1996-05-01), None
patent: 0 612 845 (1994-08-01), None
patent: 0 878 542 (1998-11-01), None
patent: 1 094 076 (2001-04-01), None
patent: 1 090 989 (2001-11-01), None
patent: WO96/05302 (1996-02-01), None
patent: WO97/11159 (1997-03-01), None
patent: WO 97/021731 (1997-06-01), None
patent: WO97/21731 (1997-06-01), None
patent: WO98/00552 (1998-01-01), None
patent: WO98/29439 (1998-07-01), None
patent: WO98/34948 (1998-08-01), None
patent: WO98/38217 (1998-09-01), None
patent: WO98/46620 (1998-10-01), None
patent: WO98/46995 (1998-10-01), None
patent: WO98/56820 (1998-12-01), None
patent: WO99/06552 (1999-02-01), None
patent: WO99/24569 (1999-05-01), None
patent: WO99/32519 (1999-07-01), None
patent: WO99/48921 (1999-09-01), None
patent: WO99/52927 (1999-10-01), None
patent: WO00/14229 (2000-03-01), None
patent: WO00/22131 (2000-04-01), None
patent: WO00/49046 (2000-08-01), None
patent: WO01/07606 (2001-02-01), None
patent: WO01/09184 (2001-02-01), None
patent: WO01/12673 (2001-02-01), None
patent: WO01/14577 (2001-03-01), None
patent: WO01/16159 (2001-03-01), None
patent: WO01/31014 (2001-05-01), None
patent: WO01/36471 (2001-05-01), None
Samama et. al., The Journal of Biological Chemistry, vol. 268, No. 7, pp. 4625-4636, 1993.
Kjelsberg et. al., The Journal of Biological Chemistry, vol. 267, No. 3, pp. 1430-1433, 1992.
Pei et al, Proc. Natl. Acad. Sci. USA. vol. 91 pp. 2699-2702,1994.
Abola, et al. EMBL Accession No. AC026756, Apr. 24, 2001.
Adams et al, EMBL Accession No. AQ001459, Aug. 24, 2001.
Birren et al, EMBL Accession No. AC027026, Apr. 27, 2000.
Birren et al, EMBL Accession No. AC011780, Oct. 18, 1999.
Birren et al, EMBL Acession No. AC016468, Dec. 1, 1999.
Boyer, et al, “Molecular cloning and expression of an avian G protein-coupledP2Y receptor,” Am. Soc. Pharmacol. Exptal. Therapeutics (1997) 928-934.
Burton et al., EMBL Accession No. A1161458, Apr. 16, 2000.
Burton, et al., EMBL Accession No. AL136106, Jan. 7, 2000.
Collier, R., EMBL Accession No. Q9NTTO, Jan. 10, 2001.
Doe Joint Genome Institute, EMBL Accession No. AC008547, Aug. 4, 1999.
Doe Joint Genome Institute, EMBL Accession No. AC008754, Aug. 4, 1999.
Doe Joint Genome Institute, EMBL Accession No. AC008728, Aug. 4, 1999.
Hattori, M., et al., EMBL Accession No. AP000808, Dec. 3, 1999.
Heise, C.E., et al., “Characterization of the human cysteinyl leukotriene 2 receptor,” J. Biological Chemistry, Sep. 29, 2000, 275(39), 30531-30536.
Kjelsberg, M.A., et al., “constitutive activation of the α1B-adrenergic receptor by all amino acid substitutions at a single site,” J. Biological Chemistry, XP-002135768, 1992, 265(3), 1430-1433.
Mahairas, G.G., et al., “Sequence-tagged connectors: A sequence approach to mapping and scanning the human genome,” Proc. Natl. Acad. Sci. USA, Aug. 1999, 96, 9739-9744.
Marchese, A., et al., “Novel GPCRs and their endogenous ligands: expanding the boundaries of physiology and pharmacology,” TiPS, Sep. 1999, 20, 370-375.
O'Dowd, B.F., et al., “Discovery of three novel G-protein-coupled receptor genes,” Genomics, XP-000863786, 1998, 310-313.
Ohono, M., et al., EMBL Accession No. AB038237, May 4, 2000.
Stadel, J.M., et al., “Orphan G protein-coupled receptors: a neglected opportunity for pioneer drug discovery,” TiPS, Nov. 1997, 18, 430-437.
Stone, N., et al., EMBL Accession No. AC007104, Apr. 23, 1999.
Wallis, J., EMBL Accession No. AL355310, May 5, 2000.
Waterson, R.H., EMBL Accession No. AC010984, Sep. 29, 1999.
Weinshank, R.H., EMBL Accession No. AC 008892, Jul. 15, 1998.
Zhao, S., et al., EMBL Accession No. AQ532303, May 18, 1999.
Shryock, John et al., “Inverse Agonists and Neutral Antagonists of Recombinant Human A1 Adenosine Receptors Stably Expressed in Chinese Hamseter Overy Cells,” Molecular Pharmacology, 1998, 53 pp. 886-893.
Wenzel-Seifert et al., “High Constitutve Activity of the Human Formyl Peptide Receptor”, Journal of Biological Chem., 1998, 273 pp. 24181-24189.
Forman, B.M., et al., “Androstane Metabolities Bind to and Deactivate the Nuclear Receptor CAR-B”, Nature, 1998 395, pp. 612-615.
Seifert R. et al., Different Effects of Gxa Splice Variants on B2-Adrenoreceptor-mediated Signaling, Journal of Biological Chem., 1998, 273, pp. 5109-5116.
Pauwels, P.J., et al., “Review: Amino Acid Domains Involved in Constitutive Activation of G-Protein-Coupled Receptors”, Molecular Neurobiology, 1998, 17 pp. 109-135.
Alla, S.A. et al., “Extracellular domains of the bradykinin B2 receptor involved in ligand binding and agonist sensing defined by anti-peptide antibodies,” J. Biol. Chem., 1996, 271, 1748-1755.
Advenier, C. et al., “Effects on the isolated human bronchus of SR 48968, a potent and selective nonpeptide antagonist of the neurokinin A (NK2) receptors,” Am. Rev. Respir. Dis., 1992, 146 (5, Pt. 1), 1177-1181.
Alexander, W.S. et a., “Point mutations within the dimer interfact homology domain of c-Mpl include constitutive receptor activity and tumorigenicity,” EMBO J., 1995, 14(22) 5569-5578.
Arvanitkis, L. et al., “Human herpesvirus KSHV encodes a constitutively actige G-protein-coupled receptor agonist activity of receptor ligands,” J. Biol. Chem. 1994, 269(16), 11687-11690.
Barker, E.L. et al., “Constitutively active 5-hydroxytryptamine 2c receptors reveal novel inverse agonist activity of receptor ligands,” J. Biol. Chem., 1994, 269(16), 11687-11690.
Baxter, G., “5-HT2 receptors: a family re-united?” Trends Pharmacol. Sci. 1995, 16, 105-110.
Besmer, P. et al., “A new acute transforming feline retrovirus and relationship of its oncogene v-kit with the protein kinase gene family,” Nature, 1986, 320, 415.
Blin, N. et al., “Mapping of single amino acid residues required for selective activation of G—by the m3 muscarinic acetylcholine reeptor,” J. Biol. Chem., 1995, 270, 17741-17748.
Bond, R.A. et al., “Inverse agonists an G-protein-coupled receptors,” in Receptor-Based Drug Design, Leff, P. (ed.), New York, M. Dekker, 1998, 363-377.
Boone, C. et al., “Mutuations that alter the third
Behan Dominic P.
Chalmers Derek T.
Liaw Chen W.
Arena Pharmaceuticals Inc.
Basi Nirmal S
Bozicevic Field & Francis LLP.
Nickol Gary B.
Scherer David C.
LandOfFree
Non-endogenous, constitutively activated human G... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Non-endogenous, constitutively activated human G..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Non-endogenous, constitutively activated human G... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4019990